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Molecules 2014, 19(7), 8788-8802; doi:10.3390/molecules19078788

Phenoxyacetohydrazide Schiff Bases: β-Glucuronidase Inhibitors

1
Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan
2
Institute of Advance Research Studies in Chemical Sciences, University of Sindh Jamshoro, Hyderabad 76080, Pakistan
3
Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, Bandar Puncak Alam, Selangor Darul Ehsan 42300, Malaysia
4
Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), Level 9, FF3, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, Bandar Puncak Alam, Selangor Darul Ehsan 42300, Malaysia
5
Faculty of Applied Science UiTM, Shah Alam, Selangor 40450, Malaysia
6
PCSIR Laboratories Complex, Shahrah-e-Dr. Salimuzzaman, Karachi 75280, Pakistan
*
Author to whom correspondence should be addressed.
Received: 7 May 2014 / Revised: 6 June 2014 / Accepted: 11 June 2014 / Published: 25 June 2014
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [332 KB, uploaded 25 June 2014]   |  

Abstract

Phenoxyacetohydrazide Schiff base analogs 128 have been synthesized and their in vitro β-glucouoronidase inhibition potential studied. Compounds 1 (IC50 = 9.20 ± 0.32 µM), 5 (IC50 = 9.47 ± 0.16 µM), 7 (IC50 = 14.7 ± 0.19 µM), 8 (IC50 = 15.4 ± 1.56 µM), 11 (IC50 = 19.6 ± 0.62 µM), 12 (IC50 = 30.7 ± 1.49 µM), 15 (IC50 = 12.0 ± 0.16 µM), 21 (IC50 = 13.7 ± 0.40 µM) and 22 (IC50 = 22.0 ± 0.14 µM) showed promising β-glucuronidase inhibition activity, better than the standard (D-saccharic acid-1,4-lactone, IC50 = 48.4 ± 1.25 µM). View Full-Text
Keywords: phenoxyacetohydrazide; Schiff bases; β-glucouoronidase; glucuronosyl-O-bonds, D-saccharic acid-1,4-lactone phenoxyacetohydrazide; Schiff bases; β-glucouoronidase; glucuronosyl-O-bonds, D-saccharic acid-1,4-lactone
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MDPI and ACS Style

Jamil, W.; Perveen, S.; Shah, S.A.A.; Taha, M.; Ismail, N.H.; Perveen, S.; Ambreen, N.; Khan, K.M.; Choudhary, M.I. Phenoxyacetohydrazide Schiff Bases: β-Glucuronidase Inhibitors. Molecules 2014, 19, 8788-8802.

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